Ramelteon Inhibitor CAS No. 196597-26-9

Cat. No.	Name	Size	Price
KI0935	Ramelteon	5 mg	$297
	Ramelteon	10 mg	$534.6
	Ramelteon	50 mg	$1600

Chemical Characteristic

Product Name	Ramelteon
Synonyms	Rozerem, TAK-375
CAS No.	196597-26-9
Molecular Weight	259.34
Formula	C₁₆H₂₁NO₂
Chemical Structure

Biological activities

Ramelteon is a selective melatonin (MT) receptor agonist. Ramelteon binds to the MT1 and MT2 receptors in the suprachiasmatic nucleus (SCN). The IC50s of ramelteon are 21.2 and 53.4 pM against human MT1 and MT2 receptors, respectively. The Ki of ramelteon is 14 and 112 pM for human MT1 and MT2 receptors in CHO cells, respectively. The maximal number of binding sites (B_{max) values of ramelteon is 555 and 133 fM/mg protein, respectively. Ramelteon reveals a 6-fold higher affinity for the MT1 receptor than that by melatonin.^[1] Ramelteon prevents pituitary adenylate cyclase-activating polypeptide-27-stimulated cAMP production with higher potency than melatonin.^[2] Ramelteon (0.03 and 0.3 mg/kg, p.o.) reveals sleep-promoting effects. The half life of ramelteon is median 1.3 hours. ^[1] Ramelteon significantly decreases wakefulness at doses of 0.001, 0.01, and 0.1 mg/kg, improves slow-wave sleep at doses of 0.001, 0.01, and 0.1 mg/kg, and increases rapid eye movement sleep at a dose of 0.1 mg/kg, compared with the vehicle controls.^[3]}

Protocols

In vivo Ramelteon is dissolved in 1% DMSO/water solution.^[1]

References

[1] Oxenkrug GF, et al. Ramelteon attenuates age-associated hypertension and weight gain in spontaneously hypertensive rats. Ann N Y Acad Sci. 2010, 1199: 114-120. 閵嗏偓閵嗏偓 [2] Nishiyama K, et al. Molecular cloning and pharmacological characterization of monkey MT1 and MT2 melatonin receptors showing high affinity for the agonist ramelteon.J Pharmacol Exp Ther. 2009, 330(3): 855-63. [3] Miyamoto M, et al. The sleep-promoting action of ramelteon (TAK-375) in freely moving cats. Sleep. 2004, 27(7): 1319-1325. 閵嗏偓閵嗏偓

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